Synthesis and evaluation of 5-HT3 receptor antagonist [11C]KF17643
β Scribed by Kiichi Ishiwata; Noriko Saito; Koji Yanagawa; Riko Furuta; Shin-Ichi Ishii; Motohiro Kiyosawa; Yoshio Homma; Kenji Ishii; Fumio Suzuki; Michio Senda
- Book ID
- 116172112
- Publisher
- Elsevier Science
- Year
- 1996
- Tongue
- English
- Weight
- 670 KB
- Volume
- 23
- Category
- Article
- ISSN
- 0969-8051
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MDL 72222, an antagonist of 5HT3 receptors, was labeled with a specific radioactivity of 340-400 mCi/mumol by alkylation of the nor-precursor with [11C]CH3I. The yield of the synthesis, starting from [11C]methyliodide to the purified product and corrected for decay, was good approximately 70-75%. Af
DR4446 (1-methyl-2a-[4-(4,5,6,7-tetrahydrothieno[3,2-c]pyridin-5-yl)butyl]-2a, 3,4,5-tetrahydro-1H-benz[cd ]indole-2-one) is a potent 5-HT 7 receptor antagonist (K i ΒΌ 9:7 nM) with a high selectivity over other 5-HT family receptors (K i for 5-HT 1A : 770 nM; for other 5-HT receptors: >1000 nM). As